Design and synthesis of 1-(benzothiazol-5-yl)-1H-1, 2, 4-triazol-5-ones as protoporphyrinogen oxidase inhibitors

…, Y Sheng-Gang, L Yan-Ping, T Ying, H Ge-Fei…

Index: Yang, Zuo; Sheng-Gang, Yang; Yan-Ping, Luo; Ying, Tan; Ge-Fei, Hao; Qiong-You, Wu; Zhen, Xi; Guang-Fu, Yang Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 11 p. 3245 - 3255

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Citation Number: 14

Abstract

Protoporphyrinogen oxidase (PPO, EC 1.3. 3.4) is the action target for several structurally diverse herbicides. A series of novel 4-(difluoromethyl)-1-(6-halo-2-substituted-benzothiazol- 5-yl)-3-methyl-1H-1, 2, 4-triazol-5 (4H)-ones 2a–z were designed and synthesized via the ring-closure of two ortho-substituents. The in vitro bioassay results indicated that the 26 newly synthesized compounds exhibited good PPO inhibition effects with Ki values ...